Fluorescence probing and molecular docking analysis of the binding interaction of bovine serum albumin (BSA) with the polarity probe AICCN.

In this work, the fluorescent probe 2-amino-4-(1H-indol-3-yl)-4H-chromene-3-carbonitrile (AICCN) has been used to evaluate its potential as a prospective polarity probe. From detailed fluorescence studies of the probe, it could be shown that AICCN can indeed function as an effective polarity probe. The calculated dipole moments of AICCN in both the ground state and excited state in various solvents lend support to the steady state fluorescence results. It was also shown that AICCN can be used to probe the micropolarity of micelles and can be used successfully for the determination of CMC of the surfactants. The binding process of the probe AICCN to BSA has been followed by plotting the binding isotherms and Scatchard Plots. The time-resolved fluorescence data indicate that the preferred binding site of AICCN in BSA lies close to the buried Trp residue Trp-213 in Domain II. This contention is further supported by the molecular docking studies. The interaction study of the probe AICCN with proteins is relevant for future use of AICCN as a hydrophobic drug. Information was also obtained about the effect of probe binding on the serum albumin structure, which may be correlated to its physiological activity. Thus, the probe AICCN can serve not only as a good reporter of polarity of the microenvironment in biological systems but also as an efficient fluorophore to monitor conformational changes in proteins in future.

Addressing the Superior Drug Delivery Performance of Bilosomes─A Microscopy and Fluorescence Study.

The global health scenario in present times has raised human awareness about drug delivery strategies. Among colloidal drug delivery vehicles, vesicular nanocarriers such as liposomes and niosomes are popular. However, liposomes and niosomes get disrupted in the harsh environment of the gastrointestinal tract. In this context, the drug delivery community has reported the superior performance of vesicles containing bile salts, that is, bilosomes. The present work attempts to examine the structural/morphological aspects underlying the superior performance of bilosomes. Optical microscopy, electron microscopy, and light scattering give a definite proof of the enhanced stability of bilosomes compared to niosomes, both prepared from the same amphiphilic molecule. Fluorescence probing of the vesicles provides detailed insight into the bilayer characteristics and the differences between bilosomes and niosomes. Fluorescence resonance energy transfer studies lend further support to the findings that bilosomes have a more flexible bilayer structure than niosomes. The entrapment efficiency of the vesicles for the well-known antioxidant curcumin (whose bioavailability is a matter of concern due to low water solubility) was also studied. Bilosomes show higher curcumin entrapment efficiency than niosomes. For use in drug delivery, one needs to establish a trade-off between cargo/drug entrapment and release. Thus, a flexible bilayer structure is an advantage.

Enhanced Hydrodynamic Radius of AOT/n-heptane/Water Reverse Micellar System Through Altered Electrostatic Interactions and Molecular Self-Assemblies.

We have demonstrated a unique approach to alter the aqueous pool size of an AOT/n-heptane/water reverse micellar system. A positively charged dye Rhodamine B (RhB) and negatively charged Rose Bengal (RB) were incorporated in the reverse micellar pool to investigate the effect of electrostatic interactions and stacking effects among the dye molecules on the AOT/n-heptane/water interface. Dynamic light scattering revealed increase in reverse micellar pool size in presence of positively charged dye aggregates at the oil-water interface. However, less expansion was observed in presence of negatively charged dye aggregates (RB). This confirms the role of electrostatic interaction in modulating the hydrodynamic radius. A head-to-tail type of stacking of RhB molecules at the interface favors this expansion. The differences in stacking of the two dyes inside the reverse micelles and their torsional mobility indicated the role of the reverse micellar interface and H-bonding ability of the microenvironment on dye aggregation. Conductivity measurements demonstrated a significant drop in percolation temperature of the reverse micellar system in presence of dye aggregates. This confirms the effect of dye aggregation and electrostatic interaction on such expansion. This strategy can be exploited for solubilizing greater amounts and a wider variety of drug molecules in microemulsions.

Copper Sulfide Nanoassemblies for Catalytic and Photoresponsive Eradication of Bacteria from Infected Wounds.

Bovine serum albumin (BSA)-encapsulated copper sulfide nanocrystals (CuS NCs) were prepared by heating an alkaline solution containing copper ions and BSA without an additional sulfur source. At a high BSA concentration (0.8 mM), nanoassembly of the as-formed CuS NCs occurs to form BSA-CuS NCs as a result of the formation of BSA gel-like structures. In addition to their intrinsic photothermal properties, the BSA-CuS NCs possess rich surface vacancies and thus exhibit enzyme-like and photodynamic activities. Spontaneous generation of hydrogen peroxide (H2O2) led to the in situ formation of copper peroxide (CPO) nanodots on the BSA-CuS NCs to catalyze singlet oxygen radical generation. The antimicrobial response was enhanced by >60-fold upon NIR laser irradiation, which was ascribed to the combined effect of the photodynamic and photothermal inactivation of bacteria. Furthermore, BSA-CuS NCs were transdermally administered onto a methicillin-resistant Staphylococcus aureus-infected wound and eradicated >99% of bacteria in just 1 min under NIR illumination due to the additional peroxidase-like activity of BSA-CuS NCs, transforming H2O2 at the infection site into hydroxyl radicals and thus increasing the synergistic effect from photodynamic and photothermal treatment. The BSA-CuS NCs exhibited insignificant in vitro cytotoxicity and hemolysis and thus can serve as highly biocompatible bactericides in preclinical applications to effectively eradicate bacteria.

Platinum ions mediate the interactions between DNA and carbon quantum dots: diagnosis of MRSA infections.

In this study, we have developed a rapid and cost-effective method employing platinum ion (Pt4+)-capped fluorescent carbon quantum dots (CQDs) coupled with loop-mediated isothermal amplification (LAMP) to detect dual MRSA genes. We synthesized nitrogen- and chlorine-co-doped fluorescent CQDs (CQDSPDs) from spermidine trihydrochloride via a simple one-step pyrolysis. The CQDSPDs capped with Pt4+ ions through the cooperative coordination of the amine and chlorine groups on the surface of CQDs facilitated the double-stranded DNA (dsDNA)-induced fluorescence quenching of CQDs, and enabled the construction of the CQDSPDs/Pt4+ probe for the detection of as few as 10 copies of the MRSA gene (mecA and femA). The sensitivity and specificity of the CQDSPDs/Pt4+ probe for MRSA detection in clinical specimens (n = 24) were 94% and 86%, respectively. Our results reveal that the CQDSPDs/Pt4+ probe has great potential for the diagnosis of antibiotic-resistant superbugs with high sensitivity, specificity, and agreement.

Carbon Dots for Bacterial Detection and Antibacterial Applications-A Minireview.

The prevention and treatment of various infections caused by microbes through antibiotics are becoming less effective due to antimicrobial resistance. Researches are focused on antimicrobial nanomaterials to inhibit bacterial growth and destroy the cells, to replace conventional antibiotics. Recently, carbon dots (C-Dots) become attractive candidates for a wide range of applications, including the detection and treatment of pathogens. In addition to low toxicity, ease of synthesis and functionalization, and high biocompatibility, C-Dots show excellent optical properties such as multi-emission, high brightness, and photostability. C-Dots have shown great potential in various fields, such as biosensing, nanomedicine, photo-catalysis, and bioimaging. This review focuses on the origin and synthesis of various C-Dots with special emphasis on bacterial detection, the antibacterial effect of CDots, and their mechanism.

"Theranostic" role of bile salt-capped silver nanoparticles - gall stone/pigment stone disruption and anticancer activity.

Silver nanoparticles (AgNPs) have been synthesized in situ in micelles formed by the bile salt sodium deoxycholate (NaDC). The AgNPs exhibit "green" fluorescence. It has been shown in the present study that they can disrupt the components of gall stones/pigment stones. This unique ability of the AgNPs has been observed upon detailed study of the interaction between the endobiotic pigment bilirubin (BR) and bile salt (NaDC). In addition, these AgNPs show significant cytotoxicity towards the breast cancer cells (MCF-7). Thus the AgNPs synthesized in this work show important physiological activity and can serve as prospective "Theranostic Materials" in future. Their green fluorescence bears relevance to future diagnostic applications while their anticancer activity and disruptive action upon BR aggregates in bile salt micelles is extremely important for therapeutic purpose. This is the first report of the use of metal nanoparticles in disruption of components of gall stones/pigment stones and thus the present work has very important physiological significance. The detailed spectral studies indicate that bile salts increase the dimerization of BR which could be linked to increased solubilisation of BR in bile salt media and consequent bile stone/pigment stone formation. Importantly, an increase in red fluorescence was observed (upon dimerization of BR), which is important for cancer detection and studying the metabolism of biological tissues.

Green synthesis of gold nanoparticles for staining human cervical cancer cells and DNA binding assay.

Gold nanoparticles have been functionalized by non-ionic surfactants (polysorbates) used in pharmaceutical formulations. This results in the formation of more well-dispersed gold nanoparticles (GNPs) than the GNPs formed in neat water. The synthesized GNPs show good temporal stability. The synthesis conditions are mild and environmentally benign. The GNPs can bind to ct-DNA and displace bound dye molecules. The DNA-binding assay is significant as it preliminarily indicated that DNA-GNP conjugates can be formed. Such conjugates are extremely promising for applications in nanobiotechnology. The GNPs can also stain the human cervical cancer (HeLa) cells over a wide concentration range while remaining non-cytotoxic, thus providing a non invasive cell staining method. This result is very promising as we observe staining of HeLa cells at very low GNP concentrations (1 µM) while the cell viability is retained even at 10-fold higher GNP concentrations.